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Synthesis
DOI: 10.1055/a-2793-0030
DOI: 10.1055/a-2793-0030
Review
Recent Advances on Asymmetric Synthesis of Benzofused Six-Membered Oxygen-Containing Heterocycles (2020–2025)
Authors
We gratefully acknowledge financial support from the Key Areas Research Program of Guangdong Provincial Department of Education (Grant No. 2024ZDZX2107, 2024ZDZX3083), Shenzhen Polytechnic University-Ruijie Oxo Synthesis R&D Center (602431002PQ) and Shenzhen Polytechnic University-TS Biotech Green Synthetic Cosmetics R&D Center (602531005PQ).
Supported by: Shenzhen Polytechnic University-TS Biotech Green Synthetic Cosmetics R&D Center 602531005PQ Supported by: Shenzhen Polytechnic University-Ruijie Oxo Synthesis R&D Center 602431002PQ
Abstract
Asymmetric synthesis due to distinct physiological effects of enantiomers has been a key focus in both academic and industrial laboratories for decades, offering challenges for chemists and enabling the development of valuable pharmaceuticals and agrochemicals. Medium-ring heterocycles, particularly benzofused oxygen-containing six-membered rings such as pyrones and pyrans, represent crucial structural motifs in synthetic and natural products and drug discovery. These scaffolds exhibit significant pharmacological activities and find additional applications in materials science, as well as in the agricultural and food industries. This review summarizes the recent advances over the past 5 years (2020–2025) in the asymmetric synthesis of valuable scaffolds such as isocoumarins, coumarins, flavonoids/chromones, and chromanes, encompassing both transition-metal-catalyzed approaches and metal-free organocatalytic strategies. It highlights the principal reaction types, strategies for stereocontrol, reported yields, and applications in synthesis of natural products.
Publication History
Received: 30 October 2025
Accepted after revision: 20 January 2026
Accepted Manuscript online:
20 January 2026
Article published online:
30 January 2026
© 2026. Thieme. All rights reserved.
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